The alkylation reaction of diethyl N‐(diphenylmethylene)aminomethylphosphonate (6) with alkyl dihalides under phase‐transfer catalysis followed by hydrolysis of the benzophenone imine moiety and subsequent cyclization provides a simple and convenient method for the synthesis of known and new cyclic α‐aminophosphonates 1–5 in moderate to good yields.
Tuberculosis is mainly treated with rifampicin, pyrazinamide, isoniazide, ethambutol and/or streptomycin; however, the first three cause hepato-and nephro-toxicity, then the patient abandons therapy. This cause contributes to the failure of the treatment and favors the appearance of drug-resistant strains. Currently, alternatives are being sought to counteract this hepatic-damage, and medicinal plants, natural compounds and/or biological products are of great interest. In this manuscript we describe current data on the hepato-protective effect from extracts of medicinal plants, compounds isolated from them and biological products that protect against liver damage caused by antitubercular (anti-TB) drugs caused by therapy in patients with tuberculosis (TB). The main consulted databases were: PubMed, Worldwidescience.org, and Scopus, including records between 2000 and 2018 years. Thus, we found many articles about hepatoprotective effect from medicinal plants and polyherbal preparations (Hepatoplus and Liv 52), the majority of these have an important effect (on preclinical study) due to their antioxidant compounds content. In addition, the hepatoprotective activity of biological products and/or natural compounds has been discussed and it should be noted that the quercetin (natural antioxidant compound)/ polyvinylpyrrolidone mixture protects against hepatic damage caused by therapy in patients with TB. Another interesting compound with good effect in TB patients is N-acetylcysteine (an oral marketed mucolytic drug) which could be repurposed as an hepatoprotective drug. We consider that these findings are of great interest for researchers and clinicians, also for the development of new agents as well as for the therapeutic use of hepatoprotective substances in patients with TB, which helps reduce the toxic effects that drugs cause.
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